1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. iGluR

iGluR

Ionotropic glutamate receptors

iGluR (ionotropic glutamate receptor) is a ligand-gated ion channel that is activated by the neurotransmitter glutamate. iGluR are integral membrane proteins compose of four large subunits that form a central ion channel pore. Sequence similarity among all known glutamate receptor subunits, including the AMPA, kainate, NMDA, and δ receptors.

AMPA receptors are the main charge carriers during basal transmission, permitting influx of sodium ions to depolarise the postsynaptic membrane. NMDA receptors are blocked by magnesium ions and therefore only permit ion flux following prior depolarisation. This enables them to act as coincidence detectors for synaptic plasticity. Calcium influx through NMDA receptors leads to persistent modifications in the strength of synaptic transmission.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B0405A
    Bupivacaine hydrochloride
    Inhibitor 99.85%
    Bupivacaine hydrochloride is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride can be used for the research of chronic pain.
    Bupivacaine hydrochloride
  • HY-13993A
    Ro 25-6981 Maleate
    Antagonist 99.25%
    Ro 25-6981 Maleate is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 Maleat shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 Maleate has the potential for the research of parkinson's disease (PD).
    Ro 25-6981 Maleate
  • HY-100806S
    Kynurenic acid-d5
    Antagonist 98.35%
    Kynurenic acid-d5 is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
    Kynurenic acid-d<sub>5</sub>
  • HY-16757
    Trofinetide
    Modulator 99.30%
    Trofinetide (NNZ-2566), a synthetic analogue of the endogenous N-terminus tripeptide, Glycine-Proline-Glutamate (GPE), has been shown to be neuroprotective in animal models of brain injury.
    Trofinetide
  • HY-100815A
    (S)-AMPA
    Agonist ≥99.0%
    (S)-AMPA (L-AMPA), an active S-enantiomer of AMPA, is a potent and selective AMPA receptor agonist.
    (S)-AMPA
  • HY-N0368
    Linalool
    Inhibitor 98.55%
    Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities.
    Linalool
  • HY-17387
    (-)-Huperzine A
    Antagonist 99.74%
    (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
    (-)-Huperzine A
  • HY-15066A
    CNQX disodium
    Antagonist 99.95%
    CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist. CNQX disodium blocks the expression of fear-potentiated startle in rats.
    CNQX disodium
  • HY-15084A
    (-)-Dizocilpine maleate
    99.92%
    (-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects.
    (-)-Dizocilpine maleate
  • HY-W018061
    Traxoprodil
    Antagonist 99.92%
    Traxoprodil (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM.
    Traxoprodil
  • HY-16940
    24(S)-Hydroxycholesterol
    Agonist 99.55%
    24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators.
    24(S)-Hydroxycholesterol
  • HY-12506
    Naspm
    Inhibitor
    Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
    Naspm
  • HY-P0117
    Tat-NR2B9c
    Inhibitor 99.77%
    Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.
    Tat-NR2B9c
  • HY-B1488
    Tacrine hydrochloride
    Inhibitor 99.95%
    Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease.
    Tacrine hydrochloride
  • HY-Y0511
    N,N-Dimethylglycine
    Agonist ≥98.0%
    N,N-Dimethylglycine (Dimethylglycine), a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine is a methyl donor that can improve immunity, act as an antioxidant to prevent oxidative stress, and scavenge excess free radicals. N,N-Dimethylglycine has antidepressant-like and surfactant effects.
    N,N-Dimethylglycine
  • HY-16312
    MDL-29951
    Antagonist 99.17%
    MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [3H]glycine binding in vitro and in vivo.
    MDL-29951
  • HY-115864
    Osavampator
    Activator 99.74%
    Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders.
    Osavampator
  • HY-101165
    Cyclothiazide
    Agonist 98.29%
    Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures.
    Cyclothiazide
  • HY-10932
    Aniracetam
    Modulator 99.94%
    Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders.
    Aniracetam
  • HY-107512
    Kynurenic acid sodium
    Antagonist 99.79%
    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
    Kynurenic acid sodium
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